Lozap Plus 30 tablets — Made in Czech Republic — Free Delivery

(Lozap Plus )
Lozap Plus 30 tablets — Made in Czech Republic — Free Delivery
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Description Lozap Plus 30 tablets — Made in Czech Republic — Free Delivery

Pharmacological properties

Lozap Plus is a combination of losartan and hydrochlorothiazide. in patients with arthritis and left ventricular hypertrophy, losartan, especially in combination with hydrochlorothiazide, reduces the risk of cardiovascular disease and mortality, which has been proven by assessing the combined incidence of cardiovascular mortality, stroke and myocardial infarction.

The components of the preparation have an additive antihypertensive effect, lowering the blood pressure level to a greater extent than each of the components separately. Due to the diuretic effect, hydrochlorothiazide increases the activity of renin in the blood plasma, stimulates the secretion of aldosterone, increases the level of angiotensin II and reduces the level of potassium in the blood plasma. Taking losartan blocks all the physiological effects of angiotensin II and, due to the inhibition of the effects of aldosterone, can help reduce the loss of potassium associated with the use of a diuretic.

Losartan has a moderate and transient uricosuric effect.

Hydrochlorothiazide slightly increases the level of uric acid in the blood; the combination of losartan and hydrochlorothiazide reduces the severity of diuretic-induced hyperuricemia.

Pharmacodynamics. Losartan. During the period of losartan administration, the elimination of negative feedback, which consists in the inhibition of renin secretion by angiotensin II, causes an increase in renin activity in the blood plasma. An increase in plasma renin is accompanied by an increase in plasma angiotensin II levels. With prolonged (6-week) treatment of patients with hypertension with losartan at a dose of 100 mg / day at the time of reaching Cmax in the blood plasma, the level of angiotensin II increased 3 times. In some patients, a higher concentration of angiotensin II was noted, especially with short treatment (2 weeks). However, antihypertensive activity and a decrease in the concentration of aldosterone in the blood plasma were manifested after 2 and 6 weeks of therapy, which indicates an effective blockade of angiotensin II receptors. The activity of renin in blood plasma and the level of angiotensin II decreased to the initial values, which were noted before the start of taking the preparation, 3 days after the discontinuation of losartan. The effect of the preparation on the activity of renin and the level of angiotensin II are comparable to those when taking 50 mg of losartan.

Since losartan is a specific antagonist of the AT1 receptors of angiotensin II, it does not inhibit ACE kininase II, an enzyme that inactivates bradykinin. A study comparing the effects of 20 and 100 mg losartan potassium with the effects of an ACE inhibitor in response to angiotensin I, II and bradykinin showed that losartan blocks the effects of angiotensin I and II without affecting the effects of bradykinin. These results correspond to the specific mechanisms of action of losartan. On the contrary, an ACE inhibitor blocks the response to angiotensin I and increases the severity of the response to bradykinin, without affecting the severity of the response to angiotensin II, which demonstrates the pharmacodynamic discrepancy between losartan and ACE inhibitors.

Plasma concentrations of losartan and its active metabolite, as well as the antihypertensive effect of losartan, increase with increasing dose of the preparation. Losartan and its active metabolite are angiotensin II receptor antagonists, as a result of which they provide an antihypertensive effect.

Pharmacokinetics. Absorption. Losartan. When taken orally, losartan is well absorbed and metabolized during the first passage through the liver, resulting in the formation of an active carboxylated metabolite and inactive metabolites. The systemic bioavailability of losartan in tablet form is about 33%. The average Cmax of losartan and its active metabolite is reached after 1 and 3-4 hours, respectively. When losartan was used during a normal meal, there was no clinically significant effect on the plasma concentration profile of losartan.

Distribution. Losartan. Losartan and its active metabolite bind to blood plasma proteins (mainly albumin) - more than 99%. The volume of distribution of losartan is 34 liters. Studies in rats have shown that losartan practically does not penetrate the BBB.

Hydrochlorothiazide. Hydrochlorothiazide crosses the placental barrier (but not the BBB) and enters breast milk.

Metabolism. Losartan. About 14% of the dose of losartan is converted to its active metabolite. After oral administration of losartan labeled with 14C, the radioactivity of the circulating blood plasma is primarily associated with the presence of losartan and its active metabolite in it.

In addition to the active metabolite, biologically inactive ones are formed, including two main metabolites, due to hydroxylation of the butyl side chain, and one minor - N-2-tetrazole-glucuronide.

Excretion. Losartan. Plasma clearance of losartan and its active metabolite is about 600 and 50 ml / min, respectively. The renal clearance of losartan and its active metabolite is about 74 and 26 ml / min, respectively. With oral administration of losartan, almost 4% of the dose is excreted unchanged in the urine and about 6% of the dose in the urine as an active metabolite. Losartan and its active metabolite have linear pharmacokinetics after oral administration of losartan at a dose of up to 200 mg.

After administration, plasma concentrations of losartan and its active metabolite decrease polyexponentially with a final T½ of about 2; 6-9 hours, respectively. When 100 mg of the preparation is taken once a day, neither losartan nor its active metabolite significantly accumulates in the blood plasma.

Losartan and its metabolites are excreted in bile and urine. After oral administration of losartan labeled with 14C, about 35% of radioactivity is detected in urine and 58% in feces.

Hydrochlorothiazide. Hydrochlorothiazide is not metabolized and is rapidly excreted by the kidneys. When the preparation level in blood plasma was monitored for at least 24 hours, T½ varied in the range of 5.6–14.8 hours. At least 61% of the dose taken was excreted unchanged for 24 hours.

Indications

Ag (in patients who are prescribed combination therapy).

Reducing the risk of cardiovascular complications and mortality in patients with hypertension and left ventricular hypertrophy.

Application

Ag. the usual initial and maintenance dose is 1 tablet once a day. in patients without an adequate therapeutic response to taking 1 tablet for 2–4 weeks, the dose of the preparation can be increased to 2 tablets once a day.

The maximum dose is 2 tablets once a day. As a rule, a stable antihypertensive effect is achieved within 3 weeks after the start of treatment.

The selection of the initial dose for elderly patients is not required.

Reducing the risk of cardiovascular complications and mortality in patients with hypertension and left ventricular hypertrophy. Patients who fail to achieve the target blood pressure when taking losartan 50 mg 1 time per day, it is necessary to choose therapy with the combined use of losartan with low doses of hydrochlorothiazide (12.5 mg). If necessary, the dose of losartan should be increased to 100 mg in combination with hydrochlorothiazide at a dose of 12.5 mg / day, then the dose should be increased to 2 tablets (only 100 mg of losartan and 25 mg of hydrochlorothiazide per day at the same time).

Lozap Plus can be administered concurrently with other antihypertensive preparations.

Lozap Plus can be used regardless of food intake. The tablet must be swallowed whole with water.

Contraindications

Hypersensitivity to the components of the preparation; anuria; hypersensitivity to sulfonamide derivatives; severe violations of the liver, kidneys; During pregnancy and breastfeeding; children under 16 years of age.

Side effects

As a result of clinical studies of the use of losartan with hydrochlorothiazide, there were no adverse events specific to this combination preparation. adverse events were limited to those previously reported with losartan and / or hydrochlorothiazide alone. the cumulative incidence of adverse events reported for this combination was compared with that for placebo. the rate of discontinuation of therapy is also comparable to that of patients taking placebo. treatment with losartan potassium and hydrochlorothiazide was well tolerated. in most cases, adverse events were mild, transient and did not require discontinuation of therapy.

In controlled clinical trials, dizziness was noted in isolated cases associated with taking the preparation. It was considered an undesirable event, the frequency of which exceeded that with placebo by more than 1%.

Losartan potassium in combination with hydrochlorothiazide is well tolerated in patients with hypertension and left ventricular hypertrophy. The most common side effects associated with taking the preparation were dizziness, general weakness, and fatigue.

In the process of post-marketing use of the preparation, the following additional adverse reactions were reported:

hypersensitivity: anaphylactic reactions, angioedema, including edema of the larynx and glottis with the development of airway obstruction and / or edema of the face, lips, larynx and / or tongue; some of these patients had a history of angioedema with other preparations, including ACE inhibitors. There are isolated reports of the development of vasculitis, including Shenlein-Henoch disease when taking losartan;

Gastrointestinal tract: there are isolated reports of the development of hepatitis, as well as diarrhea in patients who took losartan;

respiratory system: cases of cough have been reported during treatment with losartan;

skin: urticaria.

Other side effects that have been noted with the use of each of the components of the preparation, and which may be potential side effects of the preparation, are presented below.

Losartan: Rash, dose-related orthostatic effects, abdominal pain, asthenia / fatigue, chest pain, edema / swelling, palpitations, tachycardia, dyspepsia, nausea, back pain, muscle cramps, headache, insomnia, cough, nasal congestion , pharyngitis, sinusitis, upper respiratory tract infections, migraine, liver dysfunction, anemia, myalgia, pruritus.

Hydrochlorothiazide: anorexia, stomach irritation, nausea, vomiting, convulsions, diarrhea, constipation, jaundice (intrahepatic cholestatic jaundice), pancreatitis, sialoadenitis, vertigo, paresthesias, headache, xanthopsia, leukopenia, anhydrous lactic acidosis , photosensitivity, fever, necrotizing angiitis (vasculitis, cutaneous vasculitis), respiratory distress (including pneumonitis and pulmonary edema), toxic epidermal necrolysis, hyperglycemia, glucosuria, hyperuricemia, electrolyte imbalance, including hyponatremia and hypokalemia, interstitial dysfunction failure, muscle spasms, weakness, transient loss of visual acuity.

Special instructions

It is necessary to prescribe with caution to such categories of patients:

with a violation of the water and electrolyte balance (dehydration, hyponatremia, hypochloremic alkalosis, hypomagnesemia, hypokalemia), which can develop with intercurrent diarrhea or vomiting;

with bilateral stenosis of the renal arteries or stenosis of an artery of a single kidney; diabetes mellitus, hypercalcemia, hyperuricemia and / or gout; with a burdened allergic history and asthma; with systemic diseases of the connective tissue (including systemic lupus erythematosus); hypovolemia (including due to the use of diuretics in high doses); when administered simultaneously with NSAIDs, including COX-2 inhibitors.

Losartan. Impaired renal function. There are reports that in some patients who took the preparation, due to inhibition of the function of the renin-angiotensin system, changes in renal function were noted, including renal failure; these changes can be reversible and disappear after discontinuation of therapy.

Other agents that affect the renin-angiotensin system can cause an increase in blood urea and creatinine in patients with bilateral renal artery stenosis and stenosis of a solitary kidney artery.

Similar effects have been reported with losartan; these changes in renal function may be reversible and disappear after discontinuation of therapy.

Hydrochlorothiazide. Arterial hypotension and imbalance in water and electrolyte balance. As with any antihypertensive preparation, some patients may experience symptomatic hypotension. Patients should be monitored in order to timely detect clinical signs of imbalance in water and electrolyte balance, such as dehydration, hyponatremia, hypochloremic alkalosis, hypomagnesemia or hypokalemia, which may develop with intercurrent diarrhea or vomiting. In such patients, it is necessary to monitor the level of electrolytes in the blood plasma.

Metabolic and endocrine effects. Thiazide therapy can impair glucose tolerance. In some cases, it may be necessary to adjust the dose of hypoglycemic agents, including insulin.

Thiazides can reduce the excretion of calcium in the urine and cause an episodic and insignificant increase in the level of calcium in the blood plasma. Severe hypercalcemia may indicate latent hyperparathyroidism. It is necessary to stop taking a thiazide diuretic before examining the functions of the parathyroid glands.

An increase in the level of cholesterol and triglycerides in the blood may also be associated with therapy with thiazide diuretics.

In some patients, the use of thiazide diuretics can cause hyperuricemia and / or gout. Since losartan lowers uric acid levels, its combination with hydrochlorothiazide reduces the severity of diuretic-induced hyperuricemia.

Other effects. In patients using thiazide diuretics, hypersensitivity reactions can be noted even in the absence of indications of a history of allergies or asthma. There are reports of the development of exacerbation or progression of systemic lupus erythematosus with the use of thiazide diuretics.

The use of the preparation can affect the speed of psychomotor reactions.

Interactions

Losartan. in clinical studies of pharmacokinetics, no clinically significant interactions of the preparation with hydrochlorothiazide, digoxin, warfarin, cimetidine, phenobarbital, ketoconazole and erythromycin were detected. rifampin and fluconazole have been reported to reduce the level of the active metabolite. the clinical consequences of these interactions have not been studied.

The combination of losartan, like other preparations that block angiotensin II or its effects, with potassium-sparing diuretics (eg spironolactone, triamterene, amiloride), potassium-containing supplements, or potassium salts can lead to an increase in plasma potassium levels.

NSAIDs, including selective COX-2 inhibitors, can reduce the effect of diuretics and other antihypertensive preparations. Therefore, the hypotensive effect of angiotensin II receptor antagonists can be reduced by NSAIDs, including COX-2 inhibitors.

In some patients with impaired renal function who have taken NSAIDs (including COX-2 inhibitors), therapy with angiotensin II receptor antagonists may cause further deterioration of renal function. These effects are usually reversible.

Hydrochlorothiazide. With the simultaneous use of thiazide diuretics with:

ethanol, barbiturates and narcotic analgesics - the risk of orthostatic hypotension may increase;

hypoglycemic preparations (oral and insulin) - dose adjustment of hypoglycemic preparations may be required;

other antihypertensive preparations - additive effect;

cholestyramine and colestipol - in the presence of anionic exchange resins, the absorption of hydrochlorothiazide is impaired. Single doses of cholestyramine and colestipol bind hydrochlorothiazide and reduce its absorption in the gastrointestinal tract by 85 and 43%, respectively;

corticosteroids, ACTH - a marked decrease in electrolyte levels, in particular hypokalemia;

pressor amines (for example, epinephrine) - a decrease in the severity of the response to the use of pressor amines is possible, but this is not enough to exclude their use;

muscle relaxants of a non-depolarizing type of action (for example, tubocurarine) - an increase in the severity of the effect of a muscle relaxant is possible;

lithium - diuretics reduce the renal clearance of lithium and increase the risk of its toxic effect; their combined use is not recommended;

NSAIDs (including COX-2 inhibitors) - in some patients, taking NSAIDs, including selective COX-2 inhibitors, may decrease the diuretic, natriuretic and antihypertensive effects of diuretics.

The effect of the preparation on the results of laboratory tests. Due to the effect of thiazides on calcium metabolism, their intake may distort the results of studies of the function of the parathyroid glands.

Overdose

There is no data on the specific treatment of preparation overdose. in case of overdose, therapy should be discontinued, and the patient should be under medical supervision. if the preparation is recently taken, it is necessary to induce vomiting and take measures aimed at eliminating dehydration, electrolyte disturbances, hepatic coma and hypotension. treatment is symptomatic and supportive.

Losartan. Data on preparation overdose in humans are limited. The most likely manifestations of an overdose are hypotension, tachycardia; bradycardia may result from parasympathetic (vagal) stimulation. In the case of symptomatic arterial hypotension, supportive therapy is indicated. Losartan and its active metabolite are not excreted by hemodialysis.

Hydrochlorothiazide. The most commonly reported overdose symptoms are due to electrolyte deficiency (hypokalemia, hypochloremia, hyponatremia) and dehydration due to excessive urination. With the simultaneous administration of cardiac glycosides, hypokalemia can cause an increase in the severity of arrhythmias. Hydrochlorothiazide is eliminated by hemodialysis, but the extent of elimination has not been established.

Storage conditions

At a temperature not higher than 30 ° C.

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